The salvinorins serve as templates for next generation analgesics, antipruritics, and dissociative hallucinogens via selective and potent agonism of the kappa-opioid receptor (KOR). In contrast to most opioids, the salvinorins lack basic amines and bind with high affinity and selectivity via complex polyoxygenated scaffolds that have frustrated deep-seated modification by synthesis. Here we...
The salvinorins represent a unique class of polyoxygenated, non-nitrogenous diterpenes that potently and selectively modulate the kappa-opioid receptor (KOR). We recently disclosed a de novo asymmetric synthesis of this scaffold that enabled the discovery of highly potent, biased analogs, including C11-alkynes designed for the CATCH (Clearing-Assisted Tissue Click Chemistry) assay. Here, we...
The salvinorins serve as templates for next generation analgesics, antipruritics and dissociative hallucinogens via selective and potent agonism of the kappa-opioid receptor (KOR). In contrast to most opioids, the salvinorins lack basic amines and bind with high affinity and selectivity via complex polyoxygenated scaffolds that have frustrated deep-seated modification by synthesis. Here we...